Complexes of diorganotin(IV) with aminoacids and a dipeptide. Synthesis and structural investigations.

The aim of this work is to synthesize complexes of Arginine, effector of recognition, with organotin(IV) ions (R2Sn2+, R =Me, nBu) which are known to possess antitumour, antimicrobial, anti-inflammatory activities. The complexes were investigated by FT-IR and 119Sn Můssbauer.While identical stoichiometries are present for Me2Sn(Arg)2 and Me2Sn(Boc-Arg)2 complexes, 119Sn Můssbauer spectra give a clear evidence of different coordination modes. L-Arginine appears to behave as a chelating ligand through carboxylate and a-NH2 groups in the former, while in Nα-Boc-L-Arginine complex, the Nα-protected amino group being exempted from coordination, only the carboxylate groups are effectors of bondin…

Concatenazioni

Loading and release of the complex [Pt(DTBTA)(DMSO)Cl]Cl·CHCl3 with the 2,2′-dithiobis(benzothiazole) ligand into mesoporous silica and studies of antiproliferative activity on MCF-7 cells

Abstract Synthetic delivery systems have great potential for overcoming problems associated with systemic toxicity that accompanies chemotherapy with the use of cisplatin and family of platinum anticancer drugs. Mesoporous silicates have been studied in context of drug delivery and drug targeting. In this paper we report the studies of loading and release of a platinum complex, [Pt(DTBTA)(DMSO)Cl]Cl∙CHCl3 (1) where DTBTA = 2,2′-dithiobis(benzothiazole), that was recently synthesized and structurally characterized. Evaluation in vitro of antitumor activity against a human breast cancer cell line (MCF-7) showed a very potent activity of complex(1). Therefore, we thought to incorporate this co…

Organotin IV-Quinilone Antibiotic Derivatives: Solid State Investigations

Nanowire iron(III) coordination polymer based on 1,2,4-triazolo[1,5-a]pyrimidine and chloride ligands

Abstract The neutral ligand 1,2,4-triazolo[1,5-a]pyrimidine (tp) has been employed to prepare a new coordination compound of Fe(III), [FeCl3(tp)2]n (1). Compound 1 was investigated by single crystal X-ray diffraction and found to be a coordination polymer forming a ladder structure based on metal–ligand interactions, while H-bonding and aromatic interactions contribute to the supramolecular self-assembly into a 3D nanostructured material. The polymeric assembly is retained also in solution, where a metallo-supramolecular polymer based on coordinative metal–ligand binding is present, as shown by dynamic light scattering (DLS) measurements. The redox properties of the Fe(III) coordination pol…

PREPARAZIONE E CARATTERIZZAZIONE DI SISTEMI A RILASCIO CONTROLLATO PER APPLICAZIONI SU MANUFATTI DI INTERESSE STORICO-ARTISTICO

Lo scopo di questo studio è la realizzazione e lo studio di sistemi a rilascio controllato costituiti da silice mesoporosa MCM-41 e biocidi commerciali e di nuova generazione. Tali materiali possono essere utilizzati in ambito conservativo per risolvere alcuni problemi di biodeterioramento che interessano i manufatti di interesse storico-artistico e a scopo preventivo per ridurre il numero e la frequenza di interventi conservativi. La MCM-41 è stata preparata in ambiente alcalino mediante il metodo sol-gel utilizzando dei tensioattivi come templanti1. Al fine di creare un’interazione favorevole biocida-superficie, sulla superficie dei pori sono stati ancorati gruppi amminici. L’incapsulamen…

Synthesis, spectroscopic characterization and antiproliferative activity of two platinum(II) complexes containing N-donor heterocycles

Abstract Novel mononuclear complexes of Pt(II), cis -[PtCl 2 (DMSO)HL]·2DMSO ( 1 ), where HL = 7-amino-2-(methylthio)[1,2,4]triazolo[1,5- a ]pyrimidine-6-carboxylic acid and Pt(bdt)Cl 2 ( 2 ), where bdt = [2,4-bis(5,6-diphenyl-1,2,4-triazin-3yl)-pyridine] have been synthesized and characterized by elemental analysis, IR and 1 H NMR spectroscopy and X-ray crystallography diffraction analyses. The molecular structure of ( 1 ) shows that Pt(II) ion has a square planar geometry with N(3) bonded heterocycle ligand, two cis chloride anions and S-bonded dimethylsulfoxide. The antiproliferative activity of complexes ( 1 ) and ( 2 ) has been tested in vitro against HepG2 human hepatoma cells and non…

Sintesi, caratterizzazione strutturale e attività biologica in vitro di organostagno(IV) con derivati di 1,2,4-triazolo[1,5-a]pirimidina

SINTESI, CARATTERIZZAZIONE STRUTTURALE E ATTIVITÀ BIOLOGICA IN VITRO DI ORGANOSTAGNO(IV) CON DERIVATI DI 1,2,4-TRIAZOLO[1, 5-a]PIRIMIDINA Maria Assunta Girasolo a, Simona Rubino a, Piera Sabatino b aDip.to di Scienze e Tecnologie Molecolari e Biomolecolari, Università di Palermo, Viale delle Scienze, Palermo, Italy bDip.to di Chimica G. Ciamician, Università di Bologna,via F. Selmi 2, Bologna, Italy La struttura delle 1,2,4-triazolo[1,5-a]pirimidine1 è analoga a quella delle purine da cui differiscono per la presenza di un atomo di azoto pirimidinico in posizione “testa di ponte” e la scomparsa del protone acido dell’anello a cinque membri. Data la somiglianza tra questi sistemi, i composti…

ATTIVITA’ CITOTOSSICA DI COMPLESSI ORGANOSTAGNO(IV) CON TRIAZOLOPIRIMIDINE CONTENENTI ATOMI DI OSSIGENO ESOCICLICO

Le triazolopirimidine sono leganti eterociclici di crescente interesse. I composti di organostagno(IV) sono caratterizzati dalla presenza di un atomo di stagno (Sn) legato covalentemente ad uno o più sostituenti organici. In questo studio1 sono stati sintetizzati: Me3Sn(5tpO)(1); n-Bu3Sn(5tpO)(2); Me3Sn(mtpO)(3); n-Bu3Sn(mtpO)(4); n-Bu3Sn(HtpO2)(5); Ph3Sn(HtpO2)(6) e la loro citotossicità valutata su tre differenti linee cellulari tumorali umane: HCT-116 (carcinoma del colon retto), HepG2 (epatocarcinoma) e MCF-7 (carcinoma mammario). I complessi 2, 4, 5 e 6 hanno mostrato attività citotossica di 1-2 ordini di grandezza superiore al cis-platino, sulle 3 linee cellulari tumorali. Il meccanis…

Synthesis, characterization, crystal structures and in vitro antistaphylococcal activity of organotin(IV) derivatives with 5,7-disubstituted-1,2,4-triazolo[1,5-a]pyrimidine.

Abstract New organotin(IV) complexes of 5,7-ditertbutyl-1,2,4-triazolo[1,5-a]pyrimidine ( dbtp ) and 5,7-diphenyl-1,2,4-triazolo[1,5-a]pyrimidine ( dptp ) with 1:1 and/or 1:2 stoichiometry were synthesized and investigated by X-ray diffraction, FT-IR and 119 Sn Mossbauer in the solid state and by 1 H and 13 C NMR spectroscopy, in solution. Moreover, the crystal and molecular structures of Et 2 SnCl 2 (dbtp) 2 and Ph 2 SnCl 2 (EtOH) 2 (dptp) 2 are reported. The complexes contain hexacoordinated tin atoms: in Et 2 SnCl 2 (dbtp) 2 two 5,7-ditertbutyl-1,2,4-triazolo[1,5-a]pyrimidine molecules coordinate classically the tin atom through N(3) atom and the coordination around the tin atom shows a …

Organotin(IV) derivatives of fatty acids: Solid state and solution phase investigations

Polynuclear complexes of Pt(II) with polypyridyl ligands.II.Synthesis, spectroscopic and structural characterization and cytotoxic activity

Anti-cancer activity of di- and tri-organotin(IV) compounds with D-(+)-Galacturonic acid on human tumor cells

Abstract We have compared the anti-proliferative activity in vitro, of R2SnGala (1-3) [R = Me, n-Bu, Ph] and novel R3SnGala (4, 5) [R = Me, n-Bu] with D-(+)-Galacturonic acid [HGala; Galaq-, q = (2) and (1) for R2SnGala and R3SnGala, respectively] compounds, towards human tumor cell lines of intestinal carcinoma (HCT-116) and breast adenocarcinoma (MCF-7). The new synthesized 4 and 5 compounds were characterized, in solution, by 1H, 13C and 119Sn NMR, that showed that HGala acts as monoanionic moiety and evidenced the dynamic behavior of the compounds, due to inter-conversions involving the anomeric carbon atom of the ligand. Cell viability, apoptosis induction and cell cycle distribution w…

Abitare il futuro ... dopo Copenhagen. Giornate internazionali di studio alla ricerca di un nuovo modello di città

Synthesis, characterization, and cytotoxic activity of copper(II) and platinum(II) complexes of 2-benzoylpyrrole and X-ray structure of bis[2-benzoylpyrrolato(N,O)]copper(II).

Copper(II) and platinum(II) complexes of 2-benzoylpyrrole (2-BZPH) were synthesized and characterized with IR, 1 H and 1 3 C NMR spectroscopies and coordination geometry with ligands arranged in transoid fashion. The crystal structure of [Cu I I (2-BZP) 2 ] was determined by X-ray diffraction. Death of complex treated Jurkat cells was measured by flow cytometry. The bis-chelate complexes [Cu I I (2-BZP) 2 ] and [Pt I I (2-BZP) 2 ] adopt square-planar coordination geometry with ligands, arranged in transoid fashion. Concentrations of 1-10 μM Platinum(II) complexes reduced cell survival from 100% to 20%, in contrast to the copper(II) complex which caused no cell death at a concentration of 10…

Synthesis, structural characterization, anti-proliferative and antimicrobial activity of binuclear and mononuclear Pt(II) complexes with perfluoroalkyl-heterocyclic ligands

Abstract In this paper we report the synthesis of four Pt(II) complexes with 5-perfluoroalkyl-1,2,4-oxadiazolyl-pyridine and 3-perfluoroalkyl-1-methyl-1,2,4-triazolyl-pyridine ligands. Two binuclear complexes [PtCl(pfibap)2](µ-Cl)2 (1), [Pt2(µ-Cl)2(pfioap)4]Cl2 (2), and two mononuclear [PtCl2(pfptp)] (3), [PtCl2(pfhtp)2] (4), were synthesized with the ligands: 2-(5-perfluoropropyl)-1,2,4-oxadiazole-3yl)-pyridine (pfpop), 2-(5-perfluoroheptyl-1,2,4-oxadiazole-3yl)-pyridine (pfhop), 2-(3-perfluoropropyl-1-methyl-1,2,4-triazole-5yl)-pyridine (pfptp), 2-(3-perfluoroheptyl-1-methyl-1,2,4-triazole-5yl)-pyridine (pfhtp), and were structurally characterized. All complexes were tested in vitro on th…

Pt(II) complex @mesoporous silica: preparation, characterization and study of release

Cisplatin analogs, having cytotoxic activity higher than that exerted by cisplatin, have recently triggered considerable interest by the community. The cis-[PtCl2(DMSO)HL]·2DMSO, where HL = 7-amino-2-(methylthio)[1,2,4]triazolo[1,5-a]pyrimidine-6-carboxylic acid, has shown a potent cytotoxic activity on HepG2 hepatocarcinoma cells, while under identical conditions, it did not affect normal immortalized human liver cells (Chang). In this work, the above complex has been incorporated into MCM41 mesoporous silica, pure and functionalized with amino group, which is considered one of the best host for a drug delivery system for carrying high dosages of a variety of drugs in their mesopores. Sinc…

Complessi di Platinum(II): sintesi, studi di DNA-binding e loro attività antitumorale in vitro

Con lo scopo di trovare nuovi analoghi del Cis-DDP (cis-diammino dicloro platino(II)) nuovi complessi del platino sono stati sintetizzati, caratterizzati e ne è stata studiata l’attività antitumorale in vitro [1]. Recentemente sono stati preparati complessi con metalli del quarto periodo di transizione con entrambi i leganti, dipirido[3,2-a:2’,3’-c]fenazina (dppz) e glicinato (gly) [2]. I composti di nuova sintesi vengono generalmente caratterizzati attraverso parecchie tecniche analitiche incluso la cristallografia a raggi-X e la loro attività antitumorale viene testata su un vasto pannello di linee cellulari umane [1,2]. Le proprietà biologiche spesso sono correlate alla loro interazione …

Caniglia Rispoli C., Signorelli A. (a cura di), (2008), La ricerca interdisciplinare tra antropologia urbana e urbanistica. Seminario sperimentale di formazione, Guerini Editore, Milano

Cytotoxic Activity of Organotin(IV) Derivatives with Triazolopyrimidine Containing Exocyclic Oxygen Atoms

In this study cytotoxicity of organotin(IV) compounds with 1,2,4-triazolo[1,5-a]pyrimidines, Me3Sn(5tpO) (1), n-Bu3Sn(5tpO) (2), Me3Sn(mtpO) (3), n-Bu3Sn(mtpO) (4), n-Bu3Sn(HtpO2) (5), Ph3Sn(HtpO2) (6) where 5HtpO = 4,5-dihydro-5-oxo-[1,2,4]triazolo-[1,5-a]pyrimidine, HmtpO = 4,7-dihydro-5-methyl-7-oxo-[1,2,4]triazolo-[1,5-a]pyrimidine, and H2tpO2 = 4,5,6,7-tetrahydro-5,7- dioxo-[1,2,4]triazolo-[1,5-a]-pyrimidine, was assessed on three different human tumor cell lines: HCT-116 (colorectal carcinoma), HepG2 (hepatocarcinoma) and MCF-7 (breast cancer). While 1 and 3 were inactive, compounds 2, 4, 5 and 6 inhibited the growth of the three tumor cell lines with IC50 values in the submicromolar …

Complessi di Organostagno(IV) con amminoacidi e dipeptidi: sintesi, caratterizzazione e attività biologica in vitro.

Scopo della ricerca è la sintesi, caratterizzazione strutturale ed attività biologica di complessi di organostagno(IV) e amminoacidi quali L-arginina (Arg), N-Boc-L-arginina (Boc-Arg), L-ornitina (L-Orn) ed un dipeptide contenente L-arginina, Alanil-Arginina (Ala-Arg). I complessi di diorganostagno(IV) sono noti possedere attività antitumorale [1], antimicrobica [2] e antiinfiammatoria. I complessi di triorganostagno(IV) inibiscono la funzione mitocondriale almeno in tre modi: 1) reagendo con le membrane cellulari; 2) alterando lo scambio Cl-/OH- attraverso la membrana; 3) inibendo la fosforilazione ossidativa o l’idrolisi di ATP [3].L’arginina (Arg) è un amminoacido essenziale con un grup…

Synthesis, structural characterization and antitumor activity of di- and tri-organotin(IV) complexes of D-galacturonic acid

Salphen metal complexes as potential anticancer agents: interaction profile and selectivity studies toward the three G-quadruplex units in the KIT promoter

DNA G-rich sequences can organize in four-stranded structures called G-quadruplexes (G4s). These motifs are enriched in significant sites within the human genomes, including telomeres and promoters of cancer related genes. For instance, KIT proto-oncogene promoter, associated with diverse cancers, contains three adjacent G4 units, namely Kit2, SP, and Kitt. Aiming at finding new and selective G-quadruplex binders, we have synthesized and characterized five non-charged metal complexes of Pt(II), Pd(II), Ni(II), Cu(II) and Zn(II) of a chlorine substituted Salphen ligand. The crystal structure of the Pt(II) and Pd(II) complexes was determined by XRPD. FRET measurements indicated that Pt(II) an…

Incorporation of Pt(II) complex with [amino-2(methylthio)(1,2,4)triazole-(1,5-a)pyrimidine-6-carboxylic-acid] ligand in MCM41 for controlled release

Drug carriers play a critical role for the loading and the release of the drug. A promising frontier is represented by a new class of innovative medicines that represents directional transport vehicles "drug delivery" and consist of assembled structures carrier (nano)-drug. Silica-based materials, nontoxic, biocompatible, have been used as adjuvant and excipient in pharmaceutical technology. In this class of compounds, the mesoporous materials, such as MCM41, SBA-15 and hexagonal mesoporous silica, have been investigated for medication and drug delivery due to their properties. In fact, these materials show a large specific pore volume made up of regular pores having a diameter in the nanom…

Organotin(IV) derivatives with 5,7-disubstituted-1,2,4-triazolo[1,5-a]pyrimidine and their cytotoxic activities: The importance of being conformers

Abstract The organotin(IV) compounds Me2SnCl2(dbtp)(1), Me2SnCl2(dbtp)2 (2), Et2SnCl2(dbtp) (3), Et2SnCl2(dbtp)2 (4), Et2SnCl2(dptp) (5), nBu2SnCl2(dbtp)2 (6), nBu2SnCl2(dptp) (7), Ph2SnCl2(dbtp) (8), Ph2SnCl2(EtOH)2(dptp)2 (9), where dbtp = 5,7-di-tert-butyl-1,2,4-triazolo[1,5-a]pyrimidine and dptp = 5,7-diphenyl-1,2,4-triazolo [1,5-a]pyrimidine, have been tested by MTT for their cytotoxic activity on three tumor cell lines, HepG2 (human hepatocellular carcinoma), HeLa (human cervix adenocarcinoma) and MCF-7 (human breast cancer). Except for 1 and 2, which were ineffective, all compounds significantly showed a dose-dependent anti-proliferative effect against the three cell lines. By calcul…

Mononuclear Perfluoroalkyl-Heterocyclic Complexes of Pd(II): Synthesis, Structural Characterization and Antimicrobial Activity

Two mononuclear Pd(II) complexes [PdCl2(pfptp)] (1) and [PdCl2(pfhtp)] (2), with ligands 2-(3-perfluoropropyl-1-methyl-1,2,4-triazole-5yl)-pyridine (pfptp) and 2-(3-perfluoroheptyl-1-methyl-1,2,4-triazole-5yl)-pyridine (pfhtp), were synthesized and structurally characterized. The two complexes showed a bidentate coordination of the ligand occurring through N atom of pyridine ring and N4 atom of 1,2,4-triazole. Both complexes showed antimicrobial activity when tested against both Gram-negative and Gram-positive bacterial strains.

LA STRUMENTAZIONE URBANISTICA COMUNALE TRA TRADIZIONE E INNOVAZIONE. I "NUOVI" PIANI URBANISTICI COMUNALI ARTICOLATI IN DISPOSIZIONI STRUTTURALI E PROGRAMMATICHE.

Dal Piaz A., Apreda I., (2010), I tempi della pianificazione urbanistico-territoriale, Loffredo Editore, Napoli

Synthesis, structural characterisation and biological studies of new mononuclear platinum(II) complexes with sterically hindered heterocyclic ligands

Abstract Three novel cisplatin analogues were synthesized, designed according to an approach which violates the “classical” structure–activity relationship, by replacing the diamine ligands with a planar N donor heterocycle giving a sterically hindered complex. Moreover, the sterical hindrance of antitumor drug candidates potentially makes them less susceptible to deactivation by sulphur-containing proteins and helping to overcome resistance mechanisms. The resulting mononuclear complexes of sterically hindered polidentate heterocyclic N ligands [PtCl(bbp)]Cl ( 1 ) [bbp = 2,6-bis(2-benzimidazolyl)pyridine], [PtCl 2 (dptdn)](H 2 O) ( 2 ) [dptdn = sodium 5,6-diphenyl-3-(2′-pyridyl)-1,2,4-tria…

Sintesi, caratterizzazione e attività biologica di complessi di Pt(II) con leganti eterociclici azotati e solforati e legante elilenebis(ditiocarbammato).

Novel platinum(II) complexes with heterociclyc ligands: Synthesis and structural chracterization.

An array of mononuclear complexes of Pt(II) with triazine and (benzimidazolyl)pyridine heterocycles is reported. The mononuclear complexes [PtCl2(Kdptdn)] [dbtdn=5,6- diphenyl-3-(2-pyridyl)-1,2,4-triazine-4’,4’’-disulfonate sodium salt hydrate], [PtCl2(bbp)] [bbp=2,6-bis(2-benzimidazolyl)pyridine] and [PtCl2(H2dpt)]PtCl4 [dpt=5,6-diphenyl-3-(2- pyridyl)-1,2,4-triazine] have been prepared and structurally characterized. Both neutral and ionic complexes are present, with bifunctional Pt(II) moieties, whose size and shape enable them to behave as novel scaffolds for DNA binding.

L'efficacia del piano urbanistico comunale articolato in disposizioni strutturali e programmatiche. La struttura metodologica come strategia generale di ricerca

La disciplina urbanistica italiana è stata investita negli ultimi anni, a scala regionale e nazionale, da riforme legislative per il governo del territorio e da un dibattito sull’efficacia della pianificazione sempre più acceso. Queste questioni si rispecchiano all’interno della strumentazione urbanistica che, dal punto di vista applicativo, risulta sostanzialmente trasformata, nella forma e nelle procedure, ma soprattutto nell’approccio col territorio. La ricerca vuole essere un momento di riflessione critica sulla reale efficacia del modello di piano urbanistico comunale articolato in disposizioni strutturali e programmatiche, metodo innovativo di fare urbanistica a livello comunale che a…

A novel compound of triphenyltin(IV) with N-tert-butoxycarbonyl-L-ornithine causes cancer cell death by inducing a p53-dependent activation of the mitochondrial pathway of apoptosis

The triphenyltin(IV) compound with N-tert-butoxycarbonyl-L-ornithine (Boc-Orn-OH), [Ph3Sn(Boc-Orn-O)], was synthesized and characterized by elemental analysis, FT-IR, solution1H,13C and119Sn NMR and ESI mass spectrometry. The organotin(IV) compound inhibited at very low micromolar concentrations the growth of human tumor cell lines HepG2 (hepatocarcinoma cells), MCF-7 (mammary cancer) and HCT116 (colorectal carcinoma) while it did not affect the viability of non-malignant human-derived hepatic cells Chang. The mechanism of the antiproliferative effect of Ph3Sn(Boc-Orn-O), investigated on human hepatoma HepG2 cells, was pro-apoptotic, being associated with externalization of plasma membrane …

Attività anti-proliferativa di derivati di organostagno(IV) con Na-Boc-Ornitina e studio dell’azione pro-apoptotica del derivato Ph3Sn(Boc- Orn)

Nuovi composti di organostagno(IV) [R3SnL e R¢2SnL2 (R = Me, Ph e R¢= Me, nBu, HL= Na-Boc-Ornitina)] sono stati sintetizzati e caratterizzati sia allo stato solido (FT-IR) che in soluzione (1H e 13C NMR) per poterne valutare la citotossicità in linee cellulari tumorali [1]. Na-Boc-Ornitina si comporta come un legante chelante dello stagno con il gruppo carbossilato, mentre il gruppo amminico Na-protetto è esente dalla coordinazione. I composti sono stati testati per l’attività citotossica in vitro su cellule neoplastiche umane HepG2 di epatocarcinoma ed MCF7 di cancro al seno. L’effetto dei composti, nel range da 0.5 a 25 μM, dopo 24 h di incubazione è stato valutato mediante saggio MTT. Il…

Synthesis, properties, antitumor and antibacterial activity of new Pt(II) and Pd(II) complexes with 2,2′-dithiobis(benzothiazole) ligand

Mono- and binuclear Pt(II) and Pd(II) complexes with 2,20-dithiobis(benzothiazole) (DTBTA) ligand are reported. [Pt(DTBTA)(DMSO)Cl]Cl∙CHCl3 (1) and [Pd2(m-Cl)2(DTBTA)2]Cl2 (2) have been synthesized and structurally characterized by elemental analysis, IR, 1H and 13C NMR spectroscopy, MS spectrometry and the content of platinum and palladium was determined using a flame atomic spectrometer. Two different coordination modes of 1 and 2 complexes were found; in both complexes, the coordination of Pt(II) and Pd(II) ions involves the N(3) atoms of the ligand but the binuclear complex 2, is a cis-chloro-bridged palladium complex. Evaluation of their in vitro antitumor activity against two human tu…

Maintenant l'urbanistica. Discussioni e linee di ricerca per un nuovo ciclo

Palermo, Metropolitan Mainstream with a twist. Il caso palermitano presentato alla XX Conferenza INURA, Zurigo 27-30 giugno 2010

L-Arginine, Na-Boc-L-Arginine and L-Alanyl-L-Arginine complexes of Organotin(IV) ions. Synthesis and structural investigations

COMPLESSI POLINUCLEARI DI Pt(II)CON LEGANTI POLIPIRIDINICI. SINTESI, CARATTERIZZAZIONE STRUTTURALE E SPETTROSCOPICA, ATTIVITÀ CITOTOSSICA

Mono- and polynuclear complexes of Pt(II) with polypyridyl ligands. Synthesis, spectroscopic and structural characterization and cytotoxic activity.

Abstract An array of poly- and mononuclear complexes of Pt(II) with polypyridyl ligands is reported. The framework complexes [(PtCl 2 ) 2 (bpp) 2 (μ-PtCl 2 )](H 2 O) 2 [bpp = 2,3-bis(2-pyridyl)pyrazine], [PtCl 2 (μ-tptz)PtClNCPh]Cl [tptz = 2,4,6-tris(2-pyridyl)-1,3,5-triazine], and mononuclear PtCl 2 (NH 2 dpt) [NH 2 dpt = 4-amino-3,5-bis(2-pyridyl)-1,2,4-triazole] have been prepared and structurally characterized. Both neutral and ionic complexes are present, with bifunctional and monofunctional Pt(II) moieties, whose size and shape enable them to behave as novel scaffolds for DNA binding. Pt(II) complexes were tested for their biological activity. Cell viability assay and flow cytometric …

Synthetic, structural and biochemical studies of polynuclear platinum(II) complexes with heterocyclic ligands.

"Non-classical" di- and trinuclear Pt(II) complexes with polydentate nitrogen ligands; ionic [(PtCl(2))(2)(tptz)(2)(mu-PtClNCPh)]Cl (1) [tptz =2,4,6-tris(2-pyridyl)-1,3,5-triazine], [(PtCl(2))(2)(bptz)(2)(mu-Pt)]Cl(2) (2) [bptz = 3,6-bis(2-pyridyl)-1,2,4,5-tetrazine] and neutral [(PtCl(2))(2)(tptz)(2)(mu-PtCl(2))](H(2)O)(4) (3), [(PtCl(2))(2)(mu-tppz)](CHCl(3)) (4) [tppz = 2,3,5,6-tetra(2-pyridyl)pyrazine] complexes, have been prepared and structurally characterized. The neutral tptz and tppz complexes present three and two separate PtCl(2) moieties, respectively, in a cis position, presumably acting in a bifunctional mode towards DNA; the cationic tptz and bptz complexes contain monofuncti…

Quality evaluation of extra-virgin olive oils from Sicilian genotypes grown in a high-density system

Studying the sensory profile and chemical composition of monovarietal extra-virgin olive oils (EVOOs) is important to define and manage their quality and uniqueness. Chemical and sensory traits of olive oils from 14 minor Sicilian olive genotypes in comparison with oils from six major Sicilian and three international cultivars were analysed. Oils were extracted in 2015 from fruit of the 23 genotypes grown in an experimental orchard at a planting density of 1140 trees ha−1. Fatty acid composition, phenol composition, carotenoid content and antioxidant power were determined and analysed using univariate and multivariate procedures, in particular Nocellara Etnea along with carotenoid, phenol c…

New organotin(IV) complexes with L-Arginine,Nα-t-Boc-L-Arginine and L-Alanyl-L-Arginine.Synthesis, structural investigations and cytotoxic activity

Abstract Novel diorganotin(IV) derivatives of l -Arginine (HArg), N α -( tert -Butoxycarbonyl)- l -Arginine (Boc–Arg–OH) and l -Ala- l -Arg (H 2 Ala–Arg), H 2 NC( NH)NH(CH 2 ) 3 CH(NHR′)CO 2 H, where R′ = H in HArg, R′ = C(O)OC(CH 3 ) 3 in Boc–Arg–OH, R′ = H 2 NCH(CH 3 )CO in H 2 Ala–Arg and triorganotin(IV) derivatives of Boc–Arg–OH have been synthesized and structurally characterized. The complexes were investigated by FT-IR and 119 Sn Mossbauer in the solid state and by 1 H, 13 C, 119 Sn and 1 H– 1 H COSY NMR spectroscopy, in solution. The spectroscopic characterization leading to the proposed molecular structures was accomplished on the basis of these experiments. l -Arginine appears to…

Cisplatin derivative loaded in mesoporous MCM-41: preparation and characterization

The aim of this study is to design and investigate a new material constituted by mesoporous silica MCM-41 and a new cisplatin derivative, cis-PtCl2(DMSO)HL]•2DMSO, where HL = 7-amino-2-(methylthio)[1,2,4]triazolo[1,5-a]pyrimidine-6-carboxylic acid, having biological activity.[1] The high surface area and the tunable pore size of MCM-41 allow it for loading vast amounts of bioactive molecules, including biocides and drugs. Mesoporous silica MCM-41 was prepared in alkaline environment from tetraethoxysilane as Si source and cetyltrimethylammonium bromide (CTAB) as template. [2] Amino groups have been successfully grafted onto the pore surface with 3-aminopropyl triethoxysilane (APTES) in orde…

Strategie e piani di città per il Governo del territorio locale. Contributi dalla VI RUN dell’INU

Synthesis of platinum complexes with 2-(5-perfluoroalkyl-1,2,4-oxadiazol-3yl)-pyridine and 2-(3-perfluoroalkyl-1-methyl-1,2,4-triazole-5yl)-pyridine ligands and their in vitro antitumor activity.

Five new mononuclear Pt(II) complexes with 5-perfluoroalkyl-1,2,4-oxadiazolyl-pyridine and 3-perfluoroalkyl-1,2,4-triazolyl-pyridine ligands are reported. The ligands 2-(5-perfluoroheptyl-1,2,4-oxadiazole-3yl)-pyridine (pfhop), 2-(5-perfluoropropyl)-1,2,4-oxadiazole-3yl)-pyridine (pfpop), 2-(3-perfluoroheptyl-1-methyl-1,2,4-triazole-5yl)-pyridine (pfhtp), 2-(3-perfluoropropyl-1-methyl-1,2,4-triazole-5yl)-pyridine (pfptp) and their complexes [PtCl2(pfhop)(2)]center dot 1.5 DMSO (2a), [PtCl2(pfpop)(2)]center dot 1.5 DMSO (3a), [PtCl2(pfhtp)(2)]center dot 1.5 DMSO (4a), PtCl2(pfhtp) (4b), [PtCl2(PfPtP)(2)]center dot 1.5 DMSO (5a) have been synthesized and structurally characterized. The comple…

SINTESI E ATTIVITÀ PROAPOPTOTICA SU LINEE CELLULARI TUMORALI UMANE DI COMPLESSI DI Pt (II) CON LEGANTI AZOLICI FLUORURATI

Sintesi, caratterizzazione e studio dell'attività biologica di nuovi complessi mononucleari di PT(II) con leganti eterociclici

Sono stati precedentemente sintetizzati complessi mono- e polinucleari di Pt(II) [1, 2] che hanno mostrato attività citotossica maggiore del cisplatino. Tre nuovi complessi mononucleari di Pt(II) analoghi del cisplatino sono stati quindi in seguito preparati usando leganti eterociclici quali: 5,6-difenil-3-(2-piridil)-1,2,4-triazina-4’,4’’-disulfonato sodico (dptdn), 5,6-difenil-3-(2-piridil)-1,2,4-triazina (dpt) e 2,6-bis(2-benzimidazolil)piridina (bbp). I risultanti tre complessi [PtCl(bbp)]Cl (1), [PtCl2(dptdn)](H2O) (2) e [(dptdn)(dpt)Pt]Cl2(H2O) (3), ionici (1) e (3) e neutro (2), sono stati sintetizzati e strutturalmente caratterizzati tramite spettroscopia IR e NMR 1D e 2D 1H e 13C. …

CCDC 1908619: Experimental Crystal Structure Determination

Related Article: Alessandro Attanzio, Simone D’Agostino, Rosalia Busà, Anna Frazzitta, Simona Rubino, Maria Assunta Girasolo, Piera Sabatino, Luisa Tesoriere|2020|Molecules|25|859|doi:10.3390/molecules25040859

Quality evaluation of extra-virgin olive oils from Sicilian genotypes grown in a high-density system

Studying the sensory profile and chemical composition of monovarietal extra-virgin olive oils (EVOOs) is important to define and manage their quality and uniqueness. Chemical and sensory traits of olive oils from 14 minor Sicilian olive genotypes in comparison with oils from six major Sicilian and three international cultivars were analysed. Oils were extracted in 2015 from fruit of the 23 genotypes grown in an experimental orchard at a planting density of 1140 trees ha−1. Fatty acid composition, phenol composition, carotenoid content and antioxidant power were determined and analysed using univariate and multivariate procedures, in particular Nocellara Etnea along with carotenoid, phenol c…

CCDC 997203: Experimental Crystal Structure Determination

Related Article: Maria Assunta Girasolo, Alessandro Attanzio, Piera Sabatino, Luisa Tesoriere, Simona Rubino, Giancarlo Stocco|2014|Inorg.Chim.Acta|423b|168|doi:10.1016/j.ica.2014.07.015

CCDC 836072: Experimental Crystal Structure Determination

Related Article: Maria Assunta Girasolo, Loredana Canfora, Piera Sabatino, Domenico Schillaci, Elisabetta Foresti, Simona Rubino, Giuseppe Ruisi, Giancarlo Stocco|2012|J.Inorg.Biochem.|106|156|doi:10.1016/j.jinorgbio.2011.09.010

CCDC 1830492: Experimental Crystal Structure Determination

Related Article: Piera Sabatino, Simone D'Agostino, Jacopo Isopi, Simona Rubino, Massimo Marcaccio, Maria Assunta Girasolo|2019|Polyhedron|162|45|doi:10.1016/j.poly.2019.01.049

CCDC 1908620: Experimental Crystal Structure Determination

Related Article: Alessandro Attanzio, Simone D’Agostino, Rosalia Busà, Anna Frazzitta, Simona Rubino, Maria Assunta Girasolo, Piera Sabatino, Luisa Tesoriere|2020|Molecules|25|859|doi:10.3390/molecules25040859

CCDC 836073: Experimental Crystal Structure Determination

Related Article: Maria Assunta Girasolo, Loredana Canfora, Piera Sabatino, Domenico Schillaci, Elisabetta Foresti, Simona Rubino, Giuseppe Ruisi, Giancarlo Stocco|2012|J.Inorg.Biochem.|106|156|doi:10.1016/j.jinorgbio.2011.09.010